2pr3: Difference between revisions

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[[Image:2pr3.jpg|left|200px]]
{{Seed}}
[[Image:2pr3.png|left|200px]]


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{{STRUCTURE_2pr3|  PDB=2pr3  |  SCENE=  }}  
{{STRUCTURE_2pr3|  PDB=2pr3  |  SCENE=  }}  


'''Factor XA inhibitor'''
===Factor XA inhibitor===




==Overview==
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A novel series of pyrrolidine-1,2-dicarboxamides was discovered as factor Xa inhibitors using structure-based drug design. This series consisted of a neutral 4-chlorophenylurea P1, a biphenylsulfonamide P4 and a D-proline scaffold (1, IC(50) = 18 nM). Optimization of the initial hit resulted in an orally bioavailable, subnanomolar inhibitor of factor Xa (13, IC(50) = 0.38 nM), which was shown to be efficacious in a canine electrolytic model of thrombosis with minimal bleeding.
The line below this paragraph, {{ABSTRACT_PUBMED_17581239}}, adds the Publication Abstract to the page
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{{ABSTRACT_PUBMED_17581239}}


==Disease==
==Disease==
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[[Category: Blood clotting]]
[[Category: Blood clotting]]
[[Category: Fxa coagulation factor inhibitor]]
[[Category: Fxa coagulation factor inhibitor]]
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